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WO2012118812A3 - Composés hétéroaryles bicycliques substitués condensés en 6,5 - Google Patents

Composés hétéroaryles bicycliques substitués condensés en 6,5 Download PDF

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Publication number
WO2012118812A3
WO2012118812A3 PCT/US2012/026953 US2012026953W WO2012118812A3 WO 2012118812 A3 WO2012118812 A3 WO 2012118812A3 US 2012026953 W US2012026953 W US 2012026953W WO 2012118812 A3 WO2012118812 A3 WO 2012118812A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
bicyclic heteroaryl
fused bicyclic
heteroaryl compounds
compounds
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2012/026953
Other languages
English (en)
Other versions
WO2012118812A2 (fr
Inventor
Kevin Wayne Kuntz
Edward James Olhava
Richard Chesworth
Kenneth William DUNCAN
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
Original Assignee
Epizyme Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP12752135.9A priority Critical patent/EP2681216B1/fr
Priority to JP2013556804A priority patent/JP2014511389A/ja
Priority to EP17188797.9A priority patent/EP3323820B1/fr
Priority to AU2012223448A priority patent/AU2012223448B2/en
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of WO2012118812A2 publication Critical patent/WO2012118812A2/fr
Publication of WO2012118812A3 publication Critical patent/WO2012118812A3/fr
Priority to US13/938,067 priority patent/US8598167B1/en
Anticipated expiration legal-status Critical
Priority to US14/070,675 priority patent/US8962620B2/en
Priority to US14/536,162 priority patent/US9637472B2/en
Priority to US14/733,690 priority patent/US9206157B2/en
Priority to US15/492,506 priority patent/US10273223B2/en
Priority to AU2017204062A priority patent/AU2017204062A1/en
Priority to US16/299,722 priority patent/US20190300502A1/en
Priority to US16/817,791 priority patent/US20200317643A1/en
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La présente invention concerne des composés hétéroaryles bicycliques substitués condensés en 6,5. La présente invention concerne également des compositions pharmaceutiques contenant ces composés et des procédés de traitement du cancer par administration de ces composés et compositions pharmaceutiques à des sujets en ayant besoin.
PCT/US2012/026953 2011-02-28 2012-02-28 Composés hétéroaryles bicycliques substitués condensés en 6,5 Ceased WO2012118812A2 (fr)

Priority Applications (12)

Application Number Priority Date Filing Date Title
EP12752135.9A EP2681216B1 (fr) 2011-02-28 2012-02-28 Composés hétéroaryles bicycliques substitués condensés en 6,5
JP2013556804A JP2014511389A (ja) 2011-02-28 2012-02-28 置換6,5−縮合二環式ヘテロアリール化合物
EP17188797.9A EP3323820B1 (fr) 2011-02-28 2012-02-28 Composés hétéroaryles bicycliques substitués condensés en 6,5
AU2012223448A AU2012223448B2 (en) 2011-02-28 2012-02-28 Substituted 6,5-fused bicyclic heteroaryl compounds
US13/938,067 US8598167B1 (en) 2011-02-28 2013-07-09 Substituted 6,5-fused bicyclic heteroaryl compounds
US14/070,675 US8962620B2 (en) 2011-02-28 2013-11-04 Substituted 6,5-fused bicyclic heteroaryl compounds
US14/536,162 US9637472B2 (en) 2011-02-28 2014-11-07 Substituted 6,5-fused bicyclic heteroaryl compounds
US14/733,690 US9206157B2 (en) 2011-02-28 2015-06-08 Substituted 6,5-fused bicyclic heteroaryl compounds
US15/492,506 US10273223B2 (en) 2011-02-28 2017-04-20 Substituted 6,5-fused bicyclic heteroaryl compounds
AU2017204062A AU2017204062A1 (en) 2011-02-28 2017-06-15 Substituted 6,5-fused bicyclic heteroaryl compounds
US16/299,722 US20190300502A1 (en) 2011-02-28 2019-03-12 Substituted 6,5-fused bicyclic heteroaryl compounds
US16/817,791 US20200317643A1 (en) 2011-02-28 2020-03-13 Substituted 6,5-fused bicyclic heteroaryl compounds

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US201161447626P 2011-02-28 2011-02-28
US201161447632P 2011-02-28 2011-02-28
US201161447629P 2011-02-28 2011-02-28
US201161447627P 2011-02-28 2011-02-28
US201161447625P 2011-02-28 2011-02-28
US61/447,626 2011-02-28
US61/447,625 2011-02-28
US61/447,627 2011-02-28
US61/447,629 2011-02-28
US61/447,632 2011-02-28

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US13/938,067 Continuation US8598167B1 (en) 2011-02-28 2013-07-09 Substituted 6,5-fused bicyclic heteroaryl compounds

Publications (2)

Publication Number Publication Date
WO2012118812A2 WO2012118812A2 (fr) 2012-09-07
WO2012118812A3 true WO2012118812A3 (fr) 2012-11-08

Family

ID=46758456

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2012/026953 Ceased WO2012118812A2 (fr) 2011-02-28 2012-02-28 Composés hétéroaryles bicycliques substitués condensés en 6,5

Country Status (6)

Country Link
US (7) US8598167B1 (fr)
EP (2) EP3323820B1 (fr)
JP (1) JP2014511389A (fr)
AU (2) AU2012223448B2 (fr)
ES (1) ES2951688T3 (fr)
WO (1) WO2012118812A2 (fr)

Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2417127B1 (fr) 2009-04-06 2014-02-26 University Health Network Inhibiteurs de kinases et procédé de traitement du cancer avec ceux-ci
EA023173B1 (ru) 2010-04-06 2016-04-29 Юниверсити Хелс Нетворк Ингибиторы киназы и способ лечения злокачественной опухоли с их помощью
CN102970869B (zh) * 2010-05-07 2014-07-16 葛兰素史密斯克莱有限责任公司 吲哚
US8637509B2 (en) 2010-05-07 2014-01-28 Glaxosmithkline Llc Azaindazoles
EP2566328B1 (fr) 2010-05-07 2015-03-04 GlaxoSmithKline LLC Indazoles
JP6022442B2 (ja) 2010-05-14 2016-11-09 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド 男性用避妊組成物および使用方法
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
DK2571503T3 (en) 2010-05-14 2015-04-20 Dana Farber Cancer Inst Inc COMPOSITIONS AND THEIR USE IN THE TREATMENT OF NEOPLASIA, INFLAMMATORY DISEASE AND OTHER DISORDERS
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
CN103261890B (zh) 2010-09-10 2016-04-06 Epizyme股份有限公司 人ezh2抑制剂及其应用方法
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
US8765792B2 (en) 2010-12-01 2014-07-01 Glaxosmithkline Llc Indoles
EP3323820B1 (fr) 2011-02-28 2023-05-10 Epizyme, Inc. Composés hétéroaryles bicycliques substitués condensés en 6,5
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
ES2624986T3 (es) * 2011-09-13 2017-07-18 Glaxosmithkline Llc Azaindazoles
KR20140082742A (ko) 2011-09-30 2014-07-02 글락소스미스클라인 엘엘씨 암을 치료하는 방법
CN104039956A (zh) * 2011-11-04 2014-09-10 葛兰素史密斯克莱知识产权(第2号)有限公司 治疗方法
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
NZ628762A (en) * 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
JP6088491B2 (ja) 2012-04-10 2017-03-01 大日本住友製薬株式会社 新規1位置換インダゾール誘導体
CN109745316B (zh) 2012-04-13 2023-01-24 Epizyme股份有限公司 用于治疗癌症的联合治疗
PL2836491T3 (pl) 2012-04-13 2017-08-31 Epizyme, Inc. Postać soli inhibitora ludzkiej metylotransferazy histonowej EZH2
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
CA2888021A1 (fr) 2012-10-15 2014-04-24 Epizyme, Inc. Composes de n-((2-oxo-1,2-dihydropyridine-3-yl)-methyl)-benzamide substitues et leur utilisation dans le traitement de troubles medies parl'ezh2
ES2750199T3 (es) 2012-10-15 2020-03-25 Epizyme Inc Métodos para tratar el cáncer
RS56821B1 (sr) * 2012-12-19 2018-04-30 Celgene Quanticel Research Inc Inhibitori histon demetilaze
EP2935264B1 (fr) 2012-12-21 2017-10-18 Epizyme, Inc. Composés hétéroaryles bicycliques 1,4-pyridone
UA111305C2 (uk) * 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
AU2013361060B2 (en) * 2012-12-21 2018-04-19 Epizyme, Inc. 1,4-pyridone compounds
ME02730B (fr) * 2013-02-11 2017-10-20 Constellation Pharmaceuticals Inc Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (fr) 2013-03-14 2017-06-07 Epizyme, Inc. Inhibiteurs d'arginine méthyltransférase et leurs utilisations
EP2970131B1 (fr) 2013-03-14 2017-11-15 Epizyme, Inc. Inhibiteurs de l'arginine méthyltransférase et utilisations de ceux-ci
CA2903264A1 (fr) 2013-03-14 2014-11-06 Epizyme, Inc. Inhibiteurs de l'arginine methyltransferase et utilisations de ceux-ci
EP2970135B1 (fr) 2013-03-14 2018-07-18 Epizyme, Inc. Derives de pyrazol comme des inhibiteurs de prmt1 et leur utilisation
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
MX382991B (es) 2013-03-14 2025-03-13 Epizyme Inc Inhibidores de la arginina metiltransferasa y usos de los mismos.
US20160039767A1 (en) 2013-03-14 2016-02-11 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9776996B2 (en) 2013-03-15 2017-10-03 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2014151142A1 (fr) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulateurs d'enzymes de modification du méthyle, compositions et utilisations associées
US20160031907A1 (en) 2013-03-15 2016-02-04 Epizyme, Inc. Substituted Benzene Compounds
WO2014155301A1 (fr) * 2013-03-26 2014-10-02 Piramal Enterprises Limited Composés bicycliques substitués utilisés comme inhibiteurs d'ezh2
EA030196B1 (ru) * 2013-04-30 2018-07-31 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Ингибиторы энхансера zeste гомолога 2
US9556157B2 (en) 2013-07-10 2017-01-31 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
EP3022195A2 (fr) 2013-07-19 2016-05-25 Epizyme, Inc. Composés hétéroaryles bicycliques substitués condensés en 6,5
US10150764B2 (en) 2013-07-19 2018-12-11 Epizyme, Inc. Substituted benzene compounds
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
JP6088476B2 (ja) * 2013-10-08 2017-03-01 大日本住友製薬株式会社 新規1位置換インダゾール誘導体からなる医薬
PE20161273A1 (es) 2013-10-16 2016-12-18 Epizyme Inc Forma salina de hidrocloruro para la inhibicion de ezh2
CA2927612C (fr) 2013-10-18 2022-08-30 University Health Network Traitement du cancer du pancreas
CA2929652A1 (fr) 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Polytherapie pour le traitement du cancer utilisant des inhibiteurs de proteine a bromodomaine et a domaine extra-terminal (bet)
WO2015077193A1 (fr) * 2013-11-19 2015-05-28 Bristol-Myers Squibb Company Inhibiteurs de lysine méthyle transférase
WO2015077194A1 (fr) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibiteurs de la lysine méthyltransférase
MX373187B (es) 2013-12-06 2020-04-13 Epizyme Inc Terapia de combinación para tratar cáncer.
JP2017504651A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド ジアゼパン誘導体の使用
CA2936865A1 (fr) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Derives de diaminopyrimidine benzenesulfone et leurs utilisations
KR20160130778A (ko) 2014-02-28 2016-11-14 텐샤 세러퓨틱스 인코포레이티드 고인슐린혈증과 관련된 질환의 치료
KR20160122266A (ko) * 2014-03-07 2016-10-21 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 제스트 인핸서 상동체 2 억제제
AU2015240465B2 (en) 2014-04-04 2020-02-27 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
CN105037360B (zh) * 2014-04-28 2016-08-17 四川大学 吡啶酮衍生物及其制备方法和用途
BR112016029492A2 (pt) 2014-06-17 2017-10-17 Eisai R&D Man Co Ltd método para tratamento de linfoma não hodgkin
MD4820C1 (ro) 2014-06-17 2023-03-31 Pfizer Inc. Compuşi dihidroizochinolinonici substituiţi
EP3160940A4 (fr) 2014-06-25 2018-05-02 Epizyme, Inc. Composés hétéroaryles bicycliques fusionnés en 6,5 ou benzènes substitués
KR20170032474A (ko) 2014-08-08 2017-03-22 다나-파버 캔서 인스티튜트 인크. 디히드로프테리디논 유도체 및 그의 용도
JP2017526741A (ja) 2014-08-08 2017-09-14 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド ジアゼパン誘導体およびその使用
MX383635B (es) 2014-10-16 2025-03-14 Epizyme Inc Método para tratar el cáncer.
AU2015339511B2 (en) 2014-10-27 2020-05-14 Tensha Therapeutics, Inc. Bromodomain inhibitors
US11236082B2 (en) 2014-11-06 2022-02-01 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
EP3215160A4 (fr) * 2014-11-06 2018-08-08 Dana-Farber Cancer Institute, Inc. Utilisation de compositions modulant la structure de la chromatine contre la maladie du greffon contre l'hôte (gvhd)
US10786511B2 (en) 2014-11-17 2020-09-29 Epizyme, Inc. Method for treating cancer
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
WO2016102493A1 (fr) * 2014-12-22 2016-06-30 Bayer Pharma Aktiengesellschaft Inhibiteurs d'ezh2 de type imidazopyridine
EP3236962A2 (fr) 2014-12-23 2017-11-01 University of Copenhagen Traitement du cancer par inhibition de l'activité de l'ezh2
EP3285773A4 (fr) 2015-04-20 2019-04-10 Epizyme, Inc. Polythérapie pour le traitement du cancer
US20180133211A1 (en) 2015-05-19 2018-05-17 Mayo Foundation For Medical Education And Research Methods and materials for promoting bone formation
EP3307713A4 (fr) 2015-06-10 2019-01-23 Epizyme, Inc. Inhibiteurs d'ezh2 pour traiter le lymphome
WO2016201370A1 (fr) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Thérapie d'association utilisant des inhibiteurs de transcription et des inhibiteurs de kinases
UY36758A (es) * 2015-06-30 2016-12-30 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
WO2017025493A1 (fr) * 2015-08-12 2017-02-16 Bayer Pharma Aktiengesellschaft Inhibiteurs quinoléine d'ezh2
US10493076B2 (en) 2015-08-24 2019-12-03 Epizyme, Inc. Method for treating cancer
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
US10577350B2 (en) 2015-08-28 2020-03-03 Constellation Pharmaceuticals, Inc. Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
HK1256419A1 (zh) 2015-09-11 2019-09-20 达纳-法伯癌症研究所股份有限公司 乙酰胺噻吩並三唑並二氮雜環庚三烯及其用途
CA2996974A1 (fr) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Cyano-thienotriazoloazepines et leurs utilisations
US10759787B2 (en) * 2015-11-19 2020-09-01 Jiangsu Hengrui Medicine Co., Ltd. Benzofuran derivative, preparation method thereof and use thereof in medicine
CN108472295B (zh) 2015-11-25 2022-04-15 达纳-法伯癌症研究所股份有限公司 二价溴结构域抑制剂及其用途
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身tgr5促效劑之經取代之4-苯基吡啶化合物
EP3407978A4 (fr) 2016-01-29 2020-01-15 Epizyme Inc Polythérapie pour le traitement du cancer
SG10201913331VA (en) 2016-03-15 2020-03-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
JP7493304B2 (ja) 2016-04-22 2024-05-31 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド Ezh2インヒビターおよびそれらの使用
US10933068B2 (en) * 2016-05-26 2021-03-02 Sonic Master Limited Modulators of DUX4 for regulation of muscle function
JP7121660B2 (ja) 2016-06-01 2022-08-18 エピザイム,インコーポレイティド 癌を処置するためのezh2阻害剤の使用
WO2017218953A1 (fr) 2016-06-17 2017-12-21 Epizyme, Inc. Inhibiteurs d'ezh2 pour traiter le cancer
US10676479B2 (en) 2016-06-20 2020-06-09 Novartis Ag Imidazolepyridine compounds and uses thereof
EP3472161B1 (fr) 2016-06-20 2020-03-25 Novartis AG Composés de triazolopyridine et leurs utilisations
IL263429B (en) * 2016-06-20 2022-08-01 Novartis Ag Crystalline forms of triazolopyrimidine compound
CN109790160B (zh) * 2016-09-07 2022-11-15 上海海和药物研究开发股份有限公司 吡啶并五元芳香环类化合物、其制备方法及用途
EP3529242A1 (fr) 2016-10-19 2019-08-28 Constellation Pharmaceuticals, Inc. Synthèse d'inhibiteurs d'ezh2
EP3441388A1 (fr) * 2016-11-11 2019-02-13 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Dérivés indazoles 4,5,6-tri-substitués, leur préparation et leur utilisation dans des médicaments
US10793549B2 (en) * 2016-11-11 2020-10-06 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Sulfuryl-substituted benzoheterocyclic derivative, preparation method and medical use thereof
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
MY198008A (en) 2017-05-18 2023-07-25 Jiangsu Hengrui Medicine Co Crystal of benzofuran derivative free base and preparation method
US11065239B2 (en) 2017-05-18 2021-07-20 Jiangsu Hengrui Medicine Co., Ltd. Use of EZH2 inhibitor combined with BTK inhibitor in preparing drug for treating tumor
US11602529B2 (en) 2017-06-02 2023-03-14 Epizyme, Inc. Use of EZH2 inhibitors for treating cancer
WO2019050924A1 (fr) 2017-09-05 2019-03-14 Epizyme, Inc. Polythérapie pour le traitement du cancer
AU2018369841A1 (en) 2017-11-14 2020-05-07 Pfizer Inc. EZH2 inhibitor combination therapies
JP7025556B2 (ja) 2018-01-31 2022-02-24 ミラティ セラピューティクス, インコーポレイテッド Prc2阻害剤
CN110179796B (zh) * 2018-02-23 2023-01-24 江苏恒瑞医药股份有限公司 一种苯并呋喃类衍生物的组合物及制备方法
CN110229157B (zh) * 2018-03-06 2022-06-21 上海海和药物研究开发股份有限公司 嘧啶并五元芳香杂环类化合物、其制备方法及用途
EP3575287A1 (fr) * 2018-05-31 2019-12-04 Universiteit Leiden Inhibiteurs de la phospholipase d n-acylphosphatidyléthanolamine (nape-pld)
EP3823671B1 (fr) 2018-07-09 2024-02-07 Fondation Asile Des Aveugles Inhibition de sous-unités de prc2 permettant de traiter des troubles oculaires
US12390472B2 (en) 2018-07-27 2025-08-19 Evopoint Biosciences Co., Ltd. Polysubstituted benzene compound and preparation method and use thereof
KR20210097124A (ko) 2018-10-30 2021-08-06 리페어 세라퓨틱스 인크. 화합물, 약제 조성물, 및 화합물 제조 방법 및 atr 키나제 억제제로서의 이것들의 사용 방법
WO2020192650A1 (fr) 2019-03-25 2020-10-01 上海华汇拓医药科技有限公司 Procédé de préparation de composé amide et son application dans le domaine de la médecine
EP3959214A1 (fr) 2019-04-22 2022-03-02 Mirati Therapeutics, Inc. Dérivés de naphtyridine en tant qu'inhibiteurs de prc2
CN111909157B (zh) * 2019-05-07 2023-02-03 南京药石科技股份有限公司 Ezh2抑制剂及其用途
CN114269748A (zh) 2019-06-05 2022-04-01 米拉蒂医疗股份有限公司 作为用于治疗癌症的PRC2抑制剂的咪唑并[1,2-c]嘧啶衍生物
CR20220068A (es) * 2019-07-22 2022-06-30 Repare Therapeutics Inc Derivados de 2-morfolinopiridina sustituidos como inhibidores de la cinasa atr
AU2020321956A1 (en) 2019-07-31 2022-03-10 Boehringer Ingelheim International Gmbh Heterobicyclic amides as inhibitors of CD38
US20220298222A1 (en) 2019-08-22 2022-09-22 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
EP4392034A1 (fr) 2021-08-25 2024-07-03 Institut National de la Santé et de la Recherche Médicale (INSERM) Utilisation d'inhibiteurs d'ezh2 pour le traitement de la sténose aortique
CR20240147A (es) * 2021-08-30 2024-09-20 Jiangsu Hengrui Pharmaceuticals Co Ltd Uso de un inhibidor de la ezh2 en la preparación de fármacos para el tratamiento del linfoma de linfocitos t
EP4536658A1 (fr) 2022-06-13 2025-04-16 Treeline Biosciences, Inc. Agents dégradant bcl6 hétérobifonctionnels 1,8-naphthyridin-2-one
EP4536649A1 (fr) 2022-06-13 2025-04-16 Treeline Biosciences, Inc. Agents de dégradation bifonctionnels de quinolone bcl6

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080182844A1 (en) * 2005-08-04 2008-07-31 Aventis Pharma S.A. 7-Substituted Aza-Indazoles, Compositions Containing Same, Production Method and Use Thereof
US20100113415A1 (en) * 2008-05-29 2010-05-06 Rajapakse Hemaka A Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
AU694465B2 (en) 1993-12-27 1998-07-23 Eisai Co. Ltd. Anthranilic acid derivative
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
JP3906935B2 (ja) 1995-12-18 2007-04-18 杏林製薬株式会社 N−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法
YU11299A (sh) 1996-09-04 2001-07-10 Pfizer Inc. Derivati indazola
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
KR20030070082A (ko) 2000-12-28 2003-08-27 시오노기세이야쿠가부시키가이샤 칸나비노이드 2형 수용체 친화 작용을 갖는 피리돈 유도체
JPWO2003070277A1 (ja) 2002-02-19 2005-06-09 塩野義製薬株式会社 抗掻痒剤
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
WO2005014554A1 (fr) 2003-08-08 2005-02-17 Astex Therapeutics Limited Composes 1h-indazole-3-carboxamide utilises comme modulateurs de la mapkap kinase
DE602005017781D1 (de) 2004-06-01 2009-12-31 Univ North Carolina Rekonstituierter histon-methyltransferase-komplex und verfahren zur identifizierung von modulatoren dafür
KR20080080173A (ko) 2005-12-14 2008-09-02 브리스톨-마이어스 스큅 컴퍼니 세린 프로테아제 억제제로서 유용한 6-원 헤테로사이클
CN101541783B (zh) * 2006-06-30 2014-10-01 苏尼西斯制药有限公司 吡啶酮基pdk1抑制剂
US7858645B2 (en) 2006-11-01 2010-12-28 Hoffmann-La Roche Inc. Indazole derivatives
AU2008219166B2 (en) 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
WO2008104077A1 (fr) 2007-02-28 2008-09-04 Methylgene Inc. Inhibiteurs à petite molécule de protéines arginine méthyltransférases (prmt)
AP2739A (en) 2008-09-26 2013-09-30 Boehringer Ingelheim Int Azaindazole compounds as CCRI receptor antagonists
EP2566328B1 (fr) * 2010-05-07 2015-03-04 GlaxoSmithKline LLC Indazoles
US8637509B2 (en) * 2010-05-07 2014-01-28 Glaxosmithkline Llc Azaindazoles
CN102970869B (zh) * 2010-05-07 2014-07-16 葛兰素史密斯克莱有限责任公司 吲哚
CN103261890B (zh) 2010-09-10 2016-04-06 Epizyme股份有限公司 人ezh2抑制剂及其应用方法
US8765792B2 (en) 2010-12-01 2014-07-01 Glaxosmithkline Llc Indoles
EP3323820B1 (fr) 2011-02-28 2023-05-10 Epizyme, Inc. Composés hétéroaryles bicycliques substitués condensés en 6,5
GB201114051D0 (en) 2011-08-15 2011-09-28 Domainex Ltd Compounds and their uses

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080182844A1 (en) * 2005-08-04 2008-07-31 Aventis Pharma S.A. 7-Substituted Aza-Indazoles, Compositions Containing Same, Production Method and Use Thereof
US20100113415A1 (en) * 2008-05-29 2010-05-06 Rajapakse Hemaka A Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer

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US20150266854A1 (en) 2015-09-24
US20190300502A1 (en) 2019-10-03
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US20140057891A1 (en) 2014-02-27
US20180072702A1 (en) 2018-03-15
US20200317643A1 (en) 2020-10-08
US20130317026A1 (en) 2013-11-28
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